| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
ER-464195-01 (5 μM) can effectively inhibit the interaction between intracellular CRT and ITGA4 in Jurkat cells and significantly reduce the level of CRT on the cell surface [1]. ER-464195-01 (0.01-10 μM, 60 min) can inhibit the adhesion ability of PMA-stimulated VCAM-1 cells and fMLP-stimulated ICAM-1 cells, with IC50 values of 0.15 μM and 0.19 μM, respectively, but has no inhibitory effect under MnCl2 stimulation [1].
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| ln Vivo |
ER-464195-01 (5-10 mg/kg, oral, once daily for 6-32 days) improves the severity of IBD in nurses through prevention and treatment [1].
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| Animal Protocol |
Animal/Disease Models: DSS induced IBD model established in female Balb/c mice (9- to 10-week-old)[1]
Doses: 10 mg/kg (preventive administration) and 5 mg/kg (therapeutic administration) Route of Administration: Oral administration (p.o.), once daily for 6-7 days Experimental Results: Effectively alleviated the weight loss, increased DAI, and shortened colon in mice under both administration methods. Reduced the interaction signal between CRT and ITGA4. Inhibited the upregulation of key pro-inflammatory cytokine mRNAs such as TNF-α, IL1-b, IL-6, and IL-17f induced by DSS. Inhibited the phosphorylation of STAT3 (p-STAT3) induced by DSS and the production of serum amyloid A (SAA). Animal/Disease Models: CD4+CD45RBhigh T-cell transfer model established in female Balb/c mice (6-week-old)[1] Doses: 10 mg/kg Route of Administration: Oral administration (p.o.), once daily for 32 days Experimental Results: Significantly improved the weight loss in mice and the changes in their fecal characteristics (diarrhea). |
| References |
| Molecular Formula |
C23H39CLN2
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|---|---|
| Molecular Weight |
379.02
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| CAS # |
859218-37-4
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~13.19 mM; with sonication (<60°C))
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6384 mL | 13.1919 mL | 26.3838 mL | |
| 5 mM | 0.5277 mL | 2.6384 mL | 5.2768 mL | |
| 10 mM | 0.2638 mL | 1.3192 mL | 2.6384 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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